LY 333531 hydrochloride

Biological Activity

Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC₅₀ values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC₅₀ values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Preparing Stock Solutions

The following data is based on the product molecular weight 505.01. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Product Datasheets

References

References are publications that support the biological activity of the product.

Jirousek et al (1996) (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H,13H-dibenzo[e,k]]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-dione (LY333531) and related analogues: isozyme selec J.Med.Chem. 39 2664 PMID: 8709095

Faul et al (2003) Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCβ. Bioorg.Med.Chem.Lett. 13 1857 PMID: 12749884

Samokhin et al (1999) Effects of protein kinase C inhibitors on thromboxane production by thrombin-stimulated platelets. Eur.J.Pharmacol. 386 297 PMID: 10618482

Lewin et al (2018) Synthesis and Characterization of the Selective, Reversible PKC beta Inhibitor (9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione, Ruboxistaurin (LY333531) A.C.S.Chem.Neurosci.

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